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European Journal of Drug Metabolism and Pharmacokinetics

Xuan Zeng, Yang Bai, Wei Peng, Weiwei Su
BACKGROUND AND OBJECTIVES: Naringin, an active flavanone glycoside, has been widely considered as a prospective antitussive and expectorant. The present study aimed to elucidate the metabolic profile of naringin in the human body. METHODS: Four male and three female volunteers (20-30 years old and 18.8-21.7 kg/m(2) Body Mass Index) were orally administrated 320 mg naringin; their urine and feces were collected at different times and the corresponding metabolites were identified with a high resolution ultra-fast liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry (UFLC-Q-TOF-MS/MS) system...
October 15, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Yunli Yu, Quanying Zhang, Wenjun Xu, Chengzhe Lv, Gang Hao
No abstract text is available yet for this article.
October 14, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Khaled S Abdelkawy, Kelsey Lack, Fawzy Elbarbry
Up-regulation of arginase activity in several chronic disease conditions, including cancer and hypertension, may suggest new targets for treatment. Recently, the number of new arginase inhibitors with promising therapeutic effects for asthma, cancer, hypertension, diabetes mellitus, and erectile dysfunction has shown a remarkable increase. Arginase inhibitors may be chemical substances, such as boron-based amino acid derivatives, α-difluoromethylornithine (DMFO), and Nω-hydroxy-nor-L-arginine (nor-NOHA) or, of plant origin such as sauchinone, salvianolic acid B (SAB), piceatannol-3-O-β-D-glucopyranoside (PG) and obacunone...
October 12, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Mosab Arafat, Cathrin Kirchhoefer, Momir Mikov
BACKGROUND AND OBJECTIVES: Cefotaxime is a class III drug according to the Biopharmaceutical Classification System due to low intestinal permeability based on poor oral bioavailability. Bile salt compounds have been shown to be effective additive for drug permeation through several biological membranes. The main purpose of this study was to investigate the ability of a mixed micelles made of phosphatidylcholine, sodium deoxycholate, and loaded with a cefotaxime-3α,7α-dihydroxy-12-keto-5β-cholanate complex to enhance the oral bioavailability of cefotaxime in rats...
September 29, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Pahweenvaj Ratnatilaka Na Bhuket, Asma El-Magboub, Ian S Haworth, Pornchai Rojsitthisak
Curcumin is a natural product with many interesting pharmacological properties. However, these are offset by the particularly poor biopharmaceutical properties. The oral bioavailability of curcumin in humans is very low, mainly due to low solubility, poor stability, and extensive metabolism. This has led to multiple approaches to improve bioavailability, including administration of curcumin with metabolism inhibitors, formulation into nanoparticles, modification of the curcumin structure, and development of curcumin prodrugs...
September 28, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Lan-Xiang Wu, Hong-Bo Zhao, Chun-Jie Wen, Ying Li, Ying-Ying Shao, Zhu Yang, Hong-Hao Zhou
BACKGROUND AND OBJECTIVES: It is well known that the expression and function of ATP-binding cassette transporter B1 (ABCB1) show high interindividual variability, but the reasons have not yet been fully elucidated. In this study, combined influence of genetic polymorphism and DNA methylation on ABCB1 mRNA expression and digoxin pharmacokinetics in healthy Chinese males was analyzed. METHODS: A total of 93 subjects who were homozygous for the ABCB1 1236-2677-3435 TTT or CGC haplotype were enrolled in this study...
September 28, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Daping Zhang, Diana S-L Chow
Mycophenolate mofetil (MMF), an ester prodrug of mycophenolic acid (MPA), is widely used as a maintenance immunosuppressive regimen in solid organ transplant patients. It is increasingly used for the prophylaxis and treatment of graft-versus-host disease (GVHD) in hematopoietic stem cell transplantation (HSCT) patients. MPA displays extensive binding to serum albumin and glucuronidation to the inactive MPA-7-O-glucuronide (MPAG). Here, we review and discuss the pertinent information regarding the clinical pharmacokinetics of MPA in HSCT patients...
September 27, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Harilal Patel, Poonam Giri, Nuggehally R Srinivas
Goto-Kakizaki (GK) rats represent a unique non-obese and lean model with manifestation of type 2 diabetes (T2DM) broadly mimicking the human T2DM development. Therefore, in addition to the use of GK rats to test the efficacy of drugs, it may represent a great tool to study the influence of altered physiological process and/or organ specific pathophysiological changes (i.e., liver, kidney, etc.) on the disposition of drugs. The objectives of the review were: (a) to compile the published pharmacokinetic data of several drugs, such as cephalexin, cyclosporine, exendin-4, gliclazide, grepafloxacin, rosuvastatin, salsalate, salicylic acid, and theophylline, in GK rats relative to normal rats; and (b) critically evaluate the possible role of physiologically altered processes on the pharmacokinetics of reviewed drugs...
September 13, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Yoshiaki Ohtsu, Jacqueline A Gibbons, Katsuhiro Suzuki, Michael E Fitzsimmons, Kohei Nozawa, Hiroshi Arai
BACKGROUND AND OBJECTIVES: Enzalutamide is an androgen receptor inhibitor that has been approved in several countries. Absorption, distribution, metabolism, and excretion (ADME) data in animals would facilitate understanding of the efficacy and safety profiles of enzalutamide, but little information has been reported in public. The purpose of this study was to clarify the missing ADME profile in animals. METHODS: ADME of (14)C-enzalutamide after oral administration as Labrasol solution were investigated in non-fasted male Sprague-Dawley rats and beagle dogs...
September 2, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Iftekhar Mahmood
BACKGROUND AND OBJECTIVES: More than 20 million infants worldwide (15.5 % of all births) are born with low birth weight. Low birth weight is associated with poor growth in childhood and a higher incidence of adult diseases, such as type 2 diabetes, hypertension and cardiovascular disease. The objective of this study was to evaluate the predictive performance of allometric models to predict clearance, volume of distribution, and half-life in extremely low to low birth weight neonates (<1 to 2...
August 25, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Wei Wang, Hong-Jie Qian, Liang Xin, Meng-Qi Zhang, Dong-Ying Lu, Jie-Mei Jin, Gang-Yi Liu, Jing-Ying Jia, Hong-Chao Zheng, Chen Yu, Yi-Ping Wang, Fu Zhu, Yun Liu
BACKGROUND: Sulcardine sulfate is a novel antiarrhythmic agent with mechanism of action as a multi-ion channel blocker. Preclinical studies in animal models have demonstrated that sulcardine sulfate is efficacious in atrial and ventricular arrhythmias, and consequently, leads to the prevention of sudden cardiac death. OBJECTIVES: This study was conducted in healthy Chinese male subjects to investigate the pharmacokinetic profile and safety of sulcardine sulfate after repeated oral dose administration at 200, 400, and 800 mg for 5 days...
August 22, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Santiago Rojas, José Raúl Herance, Juan Domingo Gispert, Belén Arias, Ignasi Miquel, Ramón López, Pilar Sánchez, Esther Rincón, Jesús Murat
BACKGROUND AND OBJECTIVES: TT-173 is the first topical hemostatic agent based on tissue factor. To prevent thromboembolic events and intravascular coagulation it is necessary to rule out the systemic absorption of new bioactive hemostats. Here, we radiolabeled TT-173 with [(18)F]SBF to characterize its systemic absorption and biodistribution. METHODS: A group of rats were administered intravenously with [(18)F]TT-173 and were subjected to a positron emission tomography study...
August 22, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Marival Bermejo, Victor Mangas-Sanjuan, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez
β-Lapachone is a naphthoquinone with high and diverse biological activity. It is useful to treat several pathologies, in particular cancer due to its ability to induce selective apoptosis in tumoral cells. Despite its advantages, β-lapachone's clinical applications are limited by its low solubility in biological fluids and its low specific distribution pattern. In the last decade various formulation strategies have been designed and developed in order to overcome these limitations and to make feasible its wide therapeutic use...
August 18, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Devender Kodati, Harish Kaushik Kotakonda, Narsimhareddy Yellu
BACKGROUND: Olmesartan medoxomil is an orally given angiotensin II receptor antagonist indicated for the treatment of hypertension. OBJECTIVE: The aim of the study was to establish a population pharmacokinetic model for olmesartan, the active metabolite of olmesartan medoxomil, in Indian hypertensive patients, and to evaluate effects of covariates on the volume of distribution (V/F) and oral clearance (CL/F) of olmesartan. METHODS: The population pharmacokinetic model for olmesartan was developed using Phoenix NLME 1...
August 17, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Yinghong Tang, Mengkai Zheng, Yu-Lin Chen, Jianzhen Chen, Yu He
BACKGROUND AND OBJECTIVES: Ephedra alkaloids, including ephedrine (EP), pseudoephedrine (PEP) and methylephedrine (MEP), are sympathomimetic compounds with known toxicities but many Ephedra (Ephedrae herba) preparations, such as Ephedra decoction, have been clinically applied for centuries. In order to explore the possible detoxification mechanism of Ephedra alkaloids, four representative compounds in Ephedra decoction (cinnamic acid, amygdalin, glycyrrhizic acid and liquiritin) were studied for their pharmacokinetic effects on Ephedra alkaloids in Sprague-Dawley rats...
August 11, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Atsushi Kawase, Ayumi Handa, Masahiro Iwaki
BACKGROUND AND OBJECTIVES: Various nutrients modulate the expression of transporters; however, the effect of a high-cholesterol (HC) diet on the expression and function of hepatic transporters remains unclear. Here, we examined the effects of an HC diet on drug disposition via hepatic transporters, including organic anion-transporting polypeptide (Oatp), multidrug resistance-associated protein (Mrp), and bile salt export pump (Bsep). METHODS: In situ perfused rat liver system was performed...
August 10, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Jijie Li, Kewei Yan, Lisha Hou, Xudong Du, Ping Zhu, Li Zheng, Cairong Zhu
BACKGROUND AND OBJECTIVES: Pharmacokinetic/pharmacodynamic link models are widely used in dose-finding studies. By applying such models, the results of initial pharmacokinetic/pharmacodynamic studies can be used to predict the potential therapeutic dose range. This knowledge can improve the design of later comparative large-scale clinical trials by reducing the number of participants and saving time and resources. However, the modeling process can be challenging, time consuming, and costly, even when using cutting-edge, powerful pharmacological software...
August 4, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Agnieszka Karbownik, Agnieszka Bienert, Włodzimierz Płotek, Tomasz Grabowski, Magdalena Cerbin-Koczorowska, Anna Wolc, Edmund Grześkowiak
BACKGROUND AND OBJECTIVES: Paracetamol is one of the most common analgesics and antipyretics applied in health care. The aim of the study was to investigate the influence of the time-of-day administration on the paracetamol pharmacokinetics and its penetration into aqueous humour (AH). METHODS: Rabbits were divided into three groups: I-receiving paracetamol at 08.00 h, II-receiving paracetamol at 16.00 h, and III-receiving paracetamol at 24.00 h. Paracetamol was administered intravenously at a single dose of 35 mg/kg...
August 2, 2016: European Journal of Drug Metabolism and Pharmacokinetics
Baogang Xie, Huiyun Wang, Huiqin Zou, Yalan Liu, Xiangyu Kong, Xiuzhong Fang
Combination of genistein (GT) and verapamil, a P-glycoprotein (P-gp) inhibitor, can increase GT absorption in situ perfusion technology in rat. To date, little information is yet available about the effect of verapamil on oral absorption of GT in vivo. In this study, a simple and reproducible HPLC-UV method was developed and validated for determination of total GT in rat plasma. Based on this, a pharmacokinetic experiment was designed to characterize biopharmaceutical properties of GT with or without coadministration of verapamil (10...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
Suresh P Sulochana, Muzeeb Syed, Devaraj V Chandrasekar, Ramesh Mullangi, Nuggehally R Srinivas
Sucralfate, a complex of aluminium hydroxide with sulfated sucrose, forms a strong gastrointestinal tract (GIT) mucosal barrier with excellent anti-ulcer property. Because sucralfate does not undergo any significant oral absorption, sucralfate resides in the GIT for a considerable length of time. The unabsorbed sucralfate may alter the pharmacokinetics of the oral drugs by impeding its absorption and reducing the oral bioavailability. Because of the increased use of sucralfate, it was important to provide a reappraisal of the published clinical drug-drug interaction studies of sucralfate with scores of drugs...
October 2016: European Journal of Drug Metabolism and Pharmacokinetics
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